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1. 发明授权

US08278475B2 Processes for the preparation of optically active intermediates 有权
标题翻译：用于制备光学活性中间体的方法
公开(公告)号：US08278475B2
公开(公告)日：2012-10-02
申请号：US13218688
申请日：2011-08-26
申请人： Masaru Mitsuda , Tadashi Moroshima , Kentaro Tsukuya , Kazuhiko Watabe , Masahiko Yamada
发明人： Masaru Mitsuda , Tadashi Moroshima , Kentaro Tsukuya , Kazuhiko Watabe , Masahiko Yamada
IPC分类号： C07C69/635 , C07C69/743
CPC分类号： C07C51/09 , C07B2200/07 , C07C67/343 , C07C209/50 , C07C209/56 , C07C209/58 , C07C233/58 , C07C2601/02 , C07C61/40 , C07C69/753 , C07C211/35 , C07C211/40
摘要： This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl) cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1α,2α,3β(1S*,2R*),5β]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.
摘要翻译：本发明涉及制备光学活性2-（二取代芳基）环丙胺化合物和光学活性2-（二取代芳基）环丙烷甲酰胺化合物的方法，它们是制备药剂的有用中间体，特别是化合物[1S- （1α，2α，3＆bgr;（1S *，2R *），5β-[3- [2-（3,4-二氟苯基） - 环丙基]氨基] -5-（丙硫基） 2,3,5-三唑并[4,5-d]嘧啶-3-基）-5-（2-羟基乙氧基） - 环戊烷-1,2-二醇。

2. 发明授权

US08058471B2 Method for producing optically active hydroxycarboxylic acid derivatives or salts thereof 失效
标题翻译：光学活性羟基羧酸衍生物或其盐的制备方法
公开(公告)号：US08058471B2
公开(公告)日：2011-11-15
申请号：US12376803
申请日：2007-08-08
申请人： Susumu Amano , Akio Fujii , Shohei Yamamoto , Masaru Mitsuda
发明人： Susumu Amano , Akio Fujii , Shohei Yamamoto , Masaru Mitsuda
IPC分类号： C07C59/00 , C07C65/21
CPC分类号： C07B53/00 , C07B2200/07 , C07C51/00 , C07C51/367 , C07C201/12 , C07C59/48 , C07C205/56
摘要： The present invention has its object to provide a method for producing an optically active hydroxycarboxylic acid derivative which is an intermediate important for production of medicines, agrochemicals, chemical products, and so on. The production method of the present invention comprises: carrying out a hydrogen-transfer reduction of a ketocarboxylic acid or a salt thereof by the reaction of an optically active diamine complex to produce an optically active hydroxycarboxylic acid derivative. According to the present invention, it is possible to safely and efficiently produce an industrially-useful optically active hydroxycarboxylic acid derivative.
摘要翻译：本发明的目的在于提供一种光学活性羟基羧酸衍生物的制造方法，该方法是制备药物，农药，化学品等的重要中间体。本发明的制造方法包括：通过光学活性二胺配合物的反应进行酮羧酸或其盐的氢转移还原反应，生成光学活性羟基羧酸衍生物。根据本发明，可以安全有效地制备工业上有用的光学活性羟基羧酸衍生物。

3. 发明授权

US07947722B2 Imidazolidinone derivative, method of producing the same and method of producing optically active amino acid 有权
标题翻译：咪唑啉酮衍生物，其制备方法和制备光学活性氨基酸的方法
公开(公告)号：US07947722B2
公开(公告)日：2011-05-24
申请号：US12309729
申请日：2007-05-14
申请人： Yasuhiro Saka , Akio Fujii , Kazumi Okuro , Masaru Mitsuda
发明人： Yasuhiro Saka , Akio Fujii , Kazumi Okuro , Masaru Mitsuda
IPC分类号： A61K31/4166 , C07D233/32
CPC分类号： C07D233/32 , C07C227/22 , C07C231/10 , C07C229/14 , C07C229/22 , C07C229/36 , C07C237/06
摘要： The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily producing an optically active amino acid by using the derivative. The objective can be achieved by producing an optically active amino acid using a novel optically active imidazolidinone derivative represented by a general formula (3) and the like. According to the method of the present invention, an optically active imidazolidinone derivative can be obtained by preferential crystallization from a mixture of isomers of the imidazolidinone derivative. Therefore, an optically active amino acid can be easily and stereoselectively produced without cumbersome procedures required for the conventional methods, such as resolution of diastereomers, synthesis from an optically active amino acid and resolution of isomers by silica gel column chromatography.
摘要翻译：本发明的目的是提供广泛用于合成光学活性氨基酸的光学活性咪唑啉酮衍生物，易于制备衍生物的方法，以及通过使用该衍生物容易地制备光学活性氨基酸的方法。可以通过使用由通式（3）等表示的新的光学活性咪唑烷酮衍生物制造光学活性氨基酸来实现。根据本发明的方法，可以通过从咪唑烷酮衍生物的异构体的混合物中优先结晶获得光学活性咪唑烷酮衍生物。因此，光学活性氨基酸可以容易地和立体选择性地产生，而不需要常规方法所需的繁琐程序，例如拆分非对映异构体，由光学活性氨基酸的合成和通过硅胶柱色谱法拆分异构体。

4. 发明授权

US07790927B2 Processes for the preparation of optically active intermediates 失效
标题翻译：用于制备光学活性中间体的方法
公开(公告)号：US07790927B2
公开(公告)日：2010-09-07
申请号：US11833266
申请日：2007-08-03
申请人： Masaru Mitsuda , Tadashi Moroshima , Kentaro Tsukuya , Kazuhiko Watabe , Masahiko Yamada
发明人： Masaru Mitsuda , Tadashi Moroshima , Kentaro Tsukuya , Kazuhiko Watabe , Masahiko Yamada
IPC分类号： C07C209/78 , C07C209/68 , C07C231/02
CPC分类号： C07C51/09 , C07B2200/07 , C07C67/343 , C07C209/50 , C07C209/56 , C07C209/58 , C07C233/58 , C07C2601/02 , C07C61/40 , C07C69/753 , C07C211/35 , C07C211/40
摘要： This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl)cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1α,2α,3β(1S*,2R*),5β)]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.
摘要翻译：本发明涉及制备光学活性2-（二取代芳基）环丙胺化合物和光学活性2-（二取代芳基）环丙烷甲酰胺化合物的方法，它们是制备药剂的有用中间体，特别是化合物[1S- （1α，2α，3＆bgr;（1S *，2R *），5β]] - 3- [7- [2-（3,4-二氟苯基） - 环丙基]氨基] -5-（丙硫基），2,3-三唑并[4,5-d]嘧啶-3-基）-5-（2-羟基乙氧基） - 环戊烷-1,2-二醇。

5. 发明申请

US20100087643A1 METHOD FOR PRODUCING OPTICALLY ACTIVE 2-ARYLPIPERAZINE DERIVATIVE 失效
标题翻译：用于生产光学活性2-亚氨基吡啶衍生物的方法
公开(公告)号：US20100087643A1
公开(公告)日：2010-04-08
申请号：US12449460
申请日：2008-02-05
申请人： Masatoshi Ohnuki , Akira Nishiyama , Masaru Mitsuda
发明人： Masatoshi Ohnuki , Akira Nishiyama , Masaru Mitsuda
IPC分类号： C07D241/04
CPC分类号： C07B53/00 , C07D241/04
摘要： The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.
摘要翻译：本发明的目的是通过工业上可行的方法从便宜且容易获得的原料制备用作药物产品和农药的合成中间体的光学活性2-芳基哌嗪衍生物。该目的可以通过在碱的存在下用磺化剂处理由光学活性苯乙烯氧化物衍生物产生的光学活性取代的氨基二醇衍生物，然后使胺化合物反应得到2-芳基哌嗪衍生物来实现。特别地，光学活性的1-未取代-2-芳基哌嗪衍生物可以通过在过渡金属催化剂的存在下用水处理光学活性的1-烯丙基-2-芳基哌嗪衍生物来进行脱气。

6. 发明申请

US20060167282A1 Process for industrially producing optically active 1,4- benzodioxane derivative 审中-公开
标题翻译：工业生产光学活性1,4-苯并二恶烷衍生物的方法
公开(公告)号：US20060167282A1
公开(公告)日：2006-07-27
申请号：US10522734
申请日：2003-07-17
申请人： Tatsuyoshi Tanaka , Masaru Mitsuda
发明人： Tatsuyoshi Tanaka , Masaru Mitsuda
IPC分类号： C07D319/14
CPC分类号： C07D319/20
摘要： A simple and safe method for producing optically active 1,4-benzodioxane derivatives useful as intermediates for pharmaceuticals and the like from inexpensive materials is provided. An optically active triol compound (5) produced by reaction of catechol (2) and optically active 3-halogeno-1,2-propanediol (3) is sulfonylated to form optically active trisulfonate (6), followed by cyclization with a base to yield optically active 1,4-benzodioxane (1).
摘要翻译：提供了一种用于生产用作药物等的廉价材料的中间体的光学活性1,4-苯并二氧杂环戊烷衍生物的简单和安全的方法。将由邻苯二酚（2）和光学活性3-卤代-1,2-丙二醇（3）的反应制备的光学活性三醇化合物（5）磺酰化以形成光学活性三磺酸盐（6），随后用碱环化，得到光学活性1,4-苯并二恶烷（1）。

7. 发明申请

US20050014818A1 Process for producing optically active chroman derivative and intermediate 审中-公开
标题翻译：光学活性苯并二氢吡喃衍生物和中间体的制备方法
公开(公告)号：US20050014818A1
公开(公告)日：2005-01-20
申请号：US10494671
申请日：2002-11-07
申请人： Masaru Mitsuda , Tatsuyoshi Tanaka , Yoshihiko Yasohara
发明人： Masaru Mitsuda , Tatsuyoshi Tanaka , Yoshihiko Yasohara
IPC分类号： C07C39/24 , C07C303/28 , C07C303/30 , C07C309/66 , C07C309/73 , C07D311/20 , C07D405/06 , C12P7/22 , C07D311/74 , A61K31/353
CPC分类号： C07D405/06 , C07C39/24 , C07C39/245 , C07C303/28 , C07C309/66 , C07C309/73 , C07D311/20 , C12P7/22
摘要： A process for easily producing various optically active chroman derivatives that are useful as pharmaceutical intermediates from inexpensive starting materials is provided. Cyclic hemiacetal (1) obtained from dihydrocoumarin through one step is asymmetrically reduced to produce an optically active halohydrin derivative (3), and the optically active halohydrin derivative (3) is cyclized to produce an optically active chroman derivative (13):
摘要翻译：提供了一种易于制备可用作廉价起始材料的药物中间体的各种光学活性苯并二氢吡喃衍生物的方法。通过一步从二氢香豆素获得的环状半缩醛（1）被不对称地还原以产生光学活性的卤代醇衍生物（3），并将光学活性卤代醇衍生物（3）环化以产生光学活性苯并二氢吡喃衍生物（13）：

8. 发明授权

US07582781B2 Optically active halohydrin derivative and process for producing optically active epoxy alcohol derivative from the same 失效
标题翻译：光学活性卤代醇衍生物及其制备光学活性环氧醇衍生物的方法
公开(公告)号：US07582781B2
公开(公告)日：2009-09-01
申请号：US10563635
申请日：2004-07-05
申请人： Kazumi Okuro , Tatsuyoshi Tanaka , Masaru Mitsuda , Kenji Inoue
发明人： Kazumi Okuro , Tatsuyoshi Tanaka , Masaru Mitsuda , Kenji Inoue
IPC分类号： C07D301/24 , C07D301/26 , C07D405/06 , C07C33/26 , C07C69/353 , C07F7/04
CPC分类号： C07C67/29 , C07B2200/07 , C07C29/10 , C07D301/24 , C07C33/46
摘要： The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxy alcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.
摘要翻译：本发明提供了一种工业上安全，易于操作的方法，用于制备用作药物的廉价可得材料的中间体的光学活性环氧醇衍生物，并且还提供了作为环氧醇衍生物的重要中间体的新型卤代醇衍生物。此外，本发明提供了通过使卤代醇与三唑磺酰胺反应来制备三唑抗真菌剂的中间体的方法，该方法包括少量的步骤。制备光学活性环氧醇衍生物的方法包括使光学活性的α-取代的丙酸酯衍生物与卤代乙酸衍生物在碱的存在下反应以制备光学活性的卤代酮衍生物，使所得到的卤代酮衍生物与芳基金属化合物立体选择性地制备卤代醇衍生物，除去卤代醇衍生物的羟基的取代基，并用碱进行环氧化。此外，制备三唑抗真菌剂中间体的方法包括使卤代醇衍生物与三唑磺酰胺反应，该方法包括少量步骤。

9. 发明申请

US20080071114A1 Processes For The Preparation Of Optically Active Intermediates 失效
标题翻译：光学活性中间体的制备方法
公开(公告)号：US20080071114A1
公开(公告)日：2008-03-20
申请号：US11833266
申请日：2007-08-03
申请人： Masaru Mitsuda , Tadashi Moroshima , Kentaro Tsukuya , Kazuhiko Watabe , Masahiko Yamada
发明人： Masaru Mitsuda , Tadashi Moroshima , Kentaro Tsukuya , Kazuhiko Watabe , Masahiko Yamada
IPC分类号： C07C209/00
CPC分类号： C07C51/09 , C07B2200/07 , C07C67/343 , C07C209/50 , C07C209/56 , C07C209/58 , C07C233/58 , C07C2601/02 , C07C61/40 , C07C69/753 , C07C211/35 , C07C211/40
摘要： This invention relates to processes for the production of optically active 2-(disubstituted aryl)cyclopropylamine compounds and optically active 2-(disubstituted aryl)cyclopropane carboxamide compounds which are useful intermediates for the preparation of pharmaceutical agents, and in particular the compound [1S-(1α,2α,3β(1S*,2R*),5β)]-3-[7-[2-(3,4-difluorophenyl)-cyclopropyl]amino]-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl)-5-(2-hydroxyethoxy)-cyclopentane-1,2-diol.
摘要翻译：本发明涉及制备光学活性2-（二取代芳基）环丙胺化合物和光学活性2-（二取代芳基）环丙烷甲酰胺化合物的方法，它们是制备药剂的有用中间体，特别是化合物[1S- （1α，2α，3β（1S *，2R *），5β）] - 3- [7- [2-（3,4-二氟苯基） - 环丙基]氨基] -5-（丙硫基）-3H-1,2 ，3-三唑并[4,5-d]嘧啶-3-基）-5-（2-羟基乙氧基） - 环戊烷-1,2-二醇。

10. 发明授权

US07094926B2 Process for producing optically active carboxylic acid substituted in 2-position 失效
公开(公告)号：US07094926B2
公开(公告)日：2006-08-22
申请号：US10182260
申请日：2001-01-25
申请人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
发明人： Susumu Amano , Masaru Mitsuda , Kenji Inoue , Koichi Kinoshita , Koki Yamashita , Yasuyoshi Ueda
IPC分类号： C07C51/58
CPC分类号： C07C327/32 , C07C51/04 , C07C51/367 , C07C51/60 , C07C59/48 , C07C57/58 , C07C57/76
摘要： A nitrous acid salt is added at a temperature of 10 to 80° C. to an aqueous solution which contains an optically active 2-aminocarboxylic acid (4) and a protonic acid, the amount of the latter acid being 1 to 3 equivalents to the former, and which has a proton concentration of 0.5 to 2 mol/kg to conduct a reaction to thereby produce an optically active 2-hydroxycarboxylic acid (1). Thionyl chloride and a basic compound are caused to act on the compound (1) to chlorinate it and simultaneously invert the configuration in the 2-position. Thus, an optically active 2-chlorocarboxylic acid chloride (5) is induced. The compound (5) is hydrolyzed to induce an optically active 2-chlorocarboxylic acid (2). The compound (2) is reacted with a thioacetic acid salt to incorporate an acetylthio group thereinto and simultaneously invert the configuration in the 2-position to thereby produce an optically active 2-acetylthiocarboxylic acid (3).

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